theta

PKC-theta inhibitor hcl is a selective PKC-θinhibitor(IC50:12 nM).

PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)

PKC-theta inhibitor is PKC-θinhibitor, with an IC50 of 12 nM.

CTP Synthetase-IN-1 is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antitumour activity, shows anti-inflammatory activity in animal models of inflammation, inhibits human CTPS1 and human CTPS2, and can be used in studies of arthritis and rheumatoid arthritis.

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

CTP Synthetase-IN-1 Ammonium salt is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antimicrobial, anti-inflammatory and antitumor activity for the study of SARS-CoV-2 viral infections.

BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs; IC50s: 108 nM and 427 nM for B. longum BSH and B. theta BSH).

Trypanothione Synthetase-IN-1 (Compound 1) serves as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an IC50 value of 14.8 μM in the presence of the polyamine S, triamine spermidine [1].

Isoleucyl tRNA synthetase-IN-1 is a selective and potent inhibitor (Ki: 88 nM) that targets isoleucyl tRNA synthetase (IleRS).

Trypanothione Synthetase-IN-2 (Compound 3) functions as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an inhibition constant (IC50) of 5.4 μM in the presence of the polyamine S, triamine spermidine [1].

Isoleucyl tRNA synthetase-IN-2 is a selective and potent inhibitor (Ki: 114 nM) that targets isoleucyl tRNA synthetase (IleRS).

Trypanothione Synthetase-IN-3, a mixed noncompetitive inhibitor of Trypanothione Synthetase (TryS) with an inhibition constant (Ki) of 0.8 μM, is useful in researching parasites like L. infantum [1].

Acyl coenzyme A synthetase (ACS), also known as acetyl coenzyme A synthetase, plays a pivotal role in biochemical research. This enzyme catalyzes the activation of fatty acids via coenzyme A through a two-step thioesterification process, resulting in the formation of acyl coenzyme A. Subsequently, it is involved in numerous anabolic and catabolic lipid metabolism pathways and contributes to the tricarboxylic acid (TCA) cycle during aerobic respiration [1].

Trypanothione synthetase-IN-4 is a L. infantumTryS inhibitor whose activity is dependent on the concentration of the polyamine substrate. trypanothione synthetase-IN-4 exhibits a strong anti-leishmanicidal effect (EC50: 0.6 μM, SI ( Trypanothione synthetase-IN-4 can be used to study leishmaniasis.

Aminoacyl tRNA Synthetase-IN-2 (Compound 14) serves as an inhibitor of aminoacyl-tRNA synthetase (aaRS), presenting potential for the formulation of a novel class of antibiotics [1].

Epoxide hydrolases convert the EETs into vicinal diols, with the concurrent loss of much of their biological activity. The 8(S),9(R)-EET isomer is metabolized by platelet COX to form 8(S),9(R),11(R)-THETA, a trihydroxy fatty acid which may act as a renal vasoconstrictor.

Retrocyclin-1, a Theta-defensin, selectively binds to carbohydrate-rich surface molecules such as fetuin, gp120 (K d =35.4 nM), CD4 (K d =31 nM), and galactosylceramide (K d =24.1 nM) [1], thereby shielding cells from HIV-1 infection.

Lei-Dab7 TFA, a selective and high-affinity blocker of the K Ca 2.2 (SK2) channel with a dissociation constant (K d) of 3.8 nM, demonstrates over 200-fold selectivity for K Ca 2.2 compared to K Ca 2.1, K Ca 2.3, K Ca 3.1, K v, and Kir2.1. Furthermore, Lei-Dab7 TFA enhances theta-burst responses and long-term potentiation (LTP) in rat hippocampal slices in vitro.

Verosudil (AR-12286) is a highly potent Rho kinase (ROCK) inhibitor with a Ki of 2 and 2 nM against ROCK1 and ROCK2, respectively. AR-12286 reverses steroid-induced intraocular pressure in mice by decreasing intraocular pressure by increasing outflow of aqueous ether through the trabecular reticulum.

Myristoylated PKCθ pseudosubstrate peptide inhibitor is a synthetic peptide utilized to investigate the mechanism of action of protein kinase C theta (PKCθ) [1].

PolQi2, a chemical compound, effectively inhibits the helicase activity of polymerase theta (Polθ) and enhances the accuracy of gene editing across multiple loci and in various cell lines [1].

Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms. It effectively induces the translocation of nPKC-delta, -epsilon, and -theta as well as PKC-mu from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].

High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive

RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity. With an IC 50 value of 5.8 nM in the PicoGreen assay, RP-6685 effectively hinders the enzymatic activity of Polθ. In addition, it demonstrates significant antitumor efficacy as observed in a mouse tumor xenograft model [1].